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4-Amino-2-methyl-5-pyrimidinemethanamine → 4-{6-[(4-Amino-pyrimidin-5-ylmethyl)-amino]-5-bromo-pyridine-3-sulfonyl}-5-methylsulfanyl-thiophene-2-carboxamidine trifluoroacetate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-Amino-2-methyl-5-pyrimidinemethanamine | HCID 66762 | — |
| 反応物 | Trifluoroacetic acid methylene chloride | HCID 21863450 | — |
| 反応物 | tert-butyl N-[4-[(5-bromo-6-chloro-3-pyridinyl)sulfonyl]-5-methylsulfanylthiophene-2-carboximidoyl]carbamate | HCID 140043501 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 4-{6-[(4-Amino-pyrimidin-5-ylmethyl)-amino]-5-bromo-pyridine-3-sulfonyl}-5-methylsulfanyl-thiophene-2-carboxamidine trifluoroacetate | HCID 21886450 | — |
反応手順
The reaction was conducted following the procedure for Example 164: step c, using {[4-(5-bromo-6-chloro-pyridine-3-sulfonyl)-5-methylsulfanyl-thiophen-2-yl]-imino-methyl}-carbamic acid tert-butyl ester (0.035 g, 0.067 mmol), 4-amino-5-aminomethyl-2-methylpyrimidine (0.018 g, 0.135 mmol), THF [2 mL], followed by DCM/TFA (1:1) and reverse-phase HPLC to yield the title compound. ESI-MS (m/z): Calcd. for C18H19BrN6O2S3: 528.48 (M+H); found 528.0, 529.9.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07138530B2 |
| 出典データセット | uspto-grants-2006_11 |
| ORD ID | ord-092647fa57204c6da302e5245aab0d17 |
| 出典メモ | uspto-grants-2006_11 |